1,2-oxazoles (including Hydrogenated) Patents (Class 548/240)
  • Publication number: 20100279999
    Abstract: A compound of formula (I), wherein A1, A2, A3, A4, G1, L, R1, R2, R3, R4, Y1, Y2 and Y3 are as defined in claim 1; or a salt or N-oxide thereof. Furthermore, the present invention relates to processes and intermediates for preparing compounds of formula (I), to insecticidal, acaricidal, molluscicidal and nematicidal compositions comprising them and to methods of using them to combat and control insect, acarine, mollusc and nematode pests.
    Type: Application
    Filed: December 16, 2008
    Publication date: November 4, 2010
    Applicant: SYNGENTA CROP PROTECTION, INC.
    Inventors: Peter Renold, Werner Zambach, Peter Maienfisch, Michel Muehlebach
  • Publication number: 20100280248
    Abstract: Novel compounds of formula 1 or a pharmaceutically acceptable salt thereof inhibit cytochrome P450 monooxygenase.
    Type: Application
    Filed: July 12, 2010
    Publication date: November 4, 2010
    Applicant: ABBOTT LABORATORIES
    Inventor: Dale J. Kempf
  • Patent number: 7825147
    Abstract: The present invention relates to isoxazoline derivatives, which can be used as selective inhibitors of phosphodiesterase (PDE) type IV. In particular, compounds disclosed herein can be useful in the treatment of AIDS, asthma, arthritis, bronchitis, chronic obstructive pulmonary disease (COPD), psoriasis, allergic rhinitis, shock, atopic dermatitis, Crohn's disease, adult respiratory distress syndrome (ARDS), eosinophilic granuloma, allergic conjunctivitis, osteoarthritis, ulcerative colitis and other inflammatory diseases in a patient, particularly in humans. The present invention also relates to processes for the preparation of disclosed compounds, as well as pharmaceutical compositions thereof, and their use as phosphodiesterase (PDE) type IV inhibitors.
    Type: Grant
    Filed: August 30, 2004
    Date of Patent: November 2, 2010
    Assignee: Ranbaxy Laboratories Limited
    Inventors: Venkata P. Palle, Sarala Balachandran, Mohammad Salman, Gagan Kukreja, Nidhi Gupta, Abhijit Ray, Sunanda G. Dastidar
  • Publication number: 20100273832
    Abstract: A compound of formula (I): wherein A1, A2, A3, A4, G1, R1, R2, R3 and R4 are as defined in claim 1; or a salt or N-oxide thereof. Furthermore, the present invention relates to processes and intermediates for preparing compounds of Formula (I), to insecticidal, acaricidal, molluscicidal or nematicidal compositions comprising them and to methods of using them to combat and control insect, acarine, mollusc or nematode pests.
    Type: Application
    Filed: December 18, 2008
    Publication date: October 28, 2010
    Applicant: SYNGENTA CROP PROTECTION, INC.
    Inventors: Pierre Joseph Marcel Jung, Peter Renold
  • Publication number: 20100267784
    Abstract: This invention relates to novel 4,5-dihydroisoxazoles of formula (I), to their use as estrogen receptor modulators, and to methods of their preparation.
    Type: Application
    Filed: November 21, 2008
    Publication date: October 21, 2010
    Inventors: Juha Pulkkinen, Paavo Honkakoski, Mikael Peräkylä, Istvan Berczi, Reino Laatikainen
  • Patent number: 7816386
    Abstract: Cinnamic and phenylpropiolic acid derivatives of formula (I) having antitumour and chemo sensitizing activity are described. Also described are pharmaceutical compositions containing the above-mentioned compounds, for the treatment of tumours.
    Type: Grant
    Filed: May 31, 2006
    Date of Patent: October 19, 2010
    Assignee: Sigma-Tau Industrie Farmaceutiche Riunite S.p.A.
    Inventors: Claudio Pisano, Gianfranco Battistuzzi, Maria Di Marzo, Giuseppe Giannini, Mauro Marzi, Loredana Vesci, Franco Zunino, Riccardo Pezzi
  • Publication number: 20100254960
    Abstract: Disclosed are compounds of Formula 1, including all geometric and stereoisomers, N-oxides, and salts thereof, wherein R1, R2, R3, R4, R5 and R6 are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling an invertebrate pest comprising contacting the invertebrate pest or its environment with a biologically effective amount of a compound or a composition of the invention.
    Type: Application
    Filed: September 30, 2008
    Publication date: October 7, 2010
    Applicant: E. I. DuPont Nemours and Company
    Inventors: Jeffrey Keith Long, Thomas Paul Selby, Ming Xu
  • Publication number: 20100254959
    Abstract: Disclosed are compounds of Formula 1, wherein R1 is halogen, C1-C2 haloalkyl or C1-C2 haloalkoxy; R2 is H, halogen or cyano; R3 is H, halogen or CF3; R4 is H, C2-C7 alkylcarbonyl or C2-C7 alkoxycarbonyl; and R5 is C1-C6 alkyl or C1-C6 haloalkyl, each substituted with one substituent independently selected from hydroxy, C1-C6 alkoxy, C1-C6 alkylthio, C1-C6 alkylsulfinyl, C1-C6 alkylsulfonyl, C2-C7 alkylaminocarbonyl, C3-C9 dialkylaminocarbonyl, C2-C7 haloalkylaminocarbonyl and C3-C9 halodialkylaminocarbonyl. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling an invertebrate pest comprising contacting the invertebrate pest or its environment with a biologically effective amount of a compound or a composition of the invention.
    Type: Application
    Filed: June 20, 2008
    Publication date: October 7, 2010
    Applicant: E. I. DU PONT DE NEMOURS AND COMPANY
    Inventors: George Philip Lahm, Jeffrey Keith Long, Ming Xu
  • Patent number: 7807669
    Abstract: Novel biaromatic compounds having the structural formula (I) below: are formulated into pharmaceutical compositions suited for administration in human or veterinary medicine (in dermatology, and also in the fields of cardiovascular diseases, immune diseases and/or diseases associated with lipid metabolism), or, alternatively, into cosmetic compositions.
    Type: Grant
    Filed: November 6, 2008
    Date of Patent: October 5, 2010
    Assignee: Galderma Research & Development
    Inventors: Laurence Clary, Claire Bouix-Peter, Michel Rivier, Pascal Collette, Andre Jomard
  • Publication number: 20100249191
    Abstract: Novel isoxazolines of the formula (I) wherein A represents C or N; R represents haloalkyl; X represents halogen or haloalkyl; l represents 0, 1 or 2; Y represents halogen, alkyl, alkoxy, haloalkyl, cyano, nitro, amino, acylamino, alkoxycarbonylamino, haloalkoxycarbonyl-amino or alkylsulfonylamino; m represents 0, 1 or 2; and G represents any one selected from heterocyclic groups described in the specification; and intermediates, and a use thereof as insecticides and/or for controlling animal parasites.
    Type: Application
    Filed: August 1, 2007
    Publication date: September 30, 2010
    Applicant: Bayer Cropscience SA
    Inventors: Pierre-Yves Coqueron, Marie-Claire Grosjean-Cournoyer, Philippe Desbordes, Pierre Genix, Benoit Hartmann, Amos Mattes, Klaus Kunz, Rudiger Fischer, Oliver Gaertzen, Oswald Ort, Darren Mansfield, Alain Villier
  • Publication number: 20100249424
    Abstract: Disclosed is a method for preparing a compound of Formula 1 wherein R1 is CHX2, CX3, CX2CHX2 or CX2CX3; each X is independently Cl or F; Z is optionally substituted phenyl; and Q is phenyl or 1-naphthalenyl, each optionally substituted as defined in the disclosure; comprising contacting a compound of Formula 2 with hydroxylamine in the presence of a base. The present invention also relates to novel compounds of Formula 2, useful as starting materials for the aforedescribed method.
    Type: Application
    Filed: August 4, 2008
    Publication date: September 30, 2010
    Applicant: E.I.DuPont De Nemours and Company
    Inventors: Gary David Annis, Brenton Todd Smith
  • Publication number: 20100234219
    Abstract: Disclosed are compounds of Formula (1), including all geometric and stereoisomers, N-oxides, and salts thereof, Formula (1): wherein A1, A2, A3, A4, A5 and A6 are independently, selected from the group consisting of CR3 and N; provided that at most 3 of A1, A2, A3; A4, A5 and A6 is N; B1, B2 and B3 are independently selected from the group consisting of CR2. and N; each R3 is independently H, halogen, C1-C6 alkyl, C1-C6 haloalkyl, C3-C6 cycloalkyl, C3-C6 halocycloalkyl, C1-C6 alkoxy, C1-C6 haloalkoxy, C1-C6 alkylthio, C1-C6 haloalkylthio, C1-C6 alkylsulfinyl, C1-C6 haloalkylsulfinyl, C1-C6 alkylsulfonyl, C1-C6 haloalkylsulfo?yl, C1-C6 alkylamino, C2-G6 dialkylamino, —CN or —NO2; and R1, R2, R4, R5, W and n are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula (1) and methods for controlling an invertebrate pest comprising contacting the invertebrate pest or its environment with a biologically effective amount of a compound or a composition of the invention.
    Type: Application
    Filed: December 28, 2006
    Publication date: September 16, 2010
    Inventors: George Philip Lahm, Wesley Lawrence Shoop, Ming Xu
  • Publication number: 20100222392
    Abstract: A compound of formula (I) wherein A1, A2, A3, A4, R1, R2, R3 and R4 are as defined in claim 1; or a salt or N-oxide thereof. Furthermore, the present invention relates to processes and intermediates for preparing compounds of formula (I), to insecticidal, acaricidal, nematicidal or molluscicidal compositions comprising them and to methods of using them to combat and control insect, acarine, nematode or mollusc pests.
    Type: Application
    Filed: October 13, 2008
    Publication date: September 2, 2010
    Applicant: SYNGENTA CROP PROTECTION, INC.
    Inventors: Werner Zambach, Peter Renold
  • Publication number: 20100216850
    Abstract: A compound of formula (I) wherein A1, A2, A3, A4, G1, G2, R1, R2, R3, R4, Q1, Y1, Y2, Y3 and Y4 are as defined in claim 1; or a salt or TV-oxide thereof. Furthermore, the present invention relates to processes and intermediates for preparing compounds of formula (I), to insecticidal, acaricidal, nematicidal or molluscicidal compositions comprising them and to methods of using them to combat and control insect, acarine, nematode or mollusc pests.
    Type: Application
    Filed: October 13, 2008
    Publication date: August 26, 2010
    Applicant: SYNGENTA CROP PROTECTION, INC.
    Inventors: Pierre Joseph Marcel Jung, Peter Renold, Christopher Richard Ayles Godfrey, William Lutz, Peter Maienfisch, Werner Zambach
  • Patent number: 7781460
    Abstract: The present invention relates to isoxazoline derivatives of structure Ia, which can be used as selective inhibitors of phosphodiesterase (PDE) type IV. Compounds disclosed herein can be useful in the treatment of CNS disorders, AIDS, asthma, arthritis, bronchitis, chronic obstructive pulmonary disease (COPD), psoriasis, allergic rhinitis, shock, atopic dermatitis, Crohn's disease, adult respiratory distress syndrome (ARDS), eosinophilic granuloma, allergic conjunctivitis, osteoarthritis, ulcerative colitis and other inflammatory diseases especially in humans. Processes for the preparation of disclosed compounds are provided, as well as pharmaceutical compositions containing the disclosed compounds, and their use as phosphodiesterase (PDE) type IV inhibitors.
    Type: Grant
    Filed: August 30, 2006
    Date of Patent: August 24, 2010
    Assignee: Ranbaxy Laboratories Limited
    Inventors: Venkata Palle, Sarala Balachandran, Lalit Kumar Baregama, Saswati Chakladar, Sarika Ramnani, Nagarajan Muthukamal, Abhijit Ray, Sunanda G. Dastidar
  • Patent number: 7772285
    Abstract: A benzophenone derivative represented by the following formula: wherein R1 represents, for example, an optionally substituted heterocyclic group, or a substituted phenyl group; Z represents, for example, an alkylene group; R2 represents, for example, a carboxyl group optionally protected with alkyl; R3 represents, for example, an optionally protected hydroxyl group; R4 represents, for example, an optionally substituted cycloalkyloxy group; and R5 represents, for example, a hydrogen atom, or a salt thereof has anti-arthritic activity, inhibits bone destruction caused by arthritis, and provides high safety and excellent pharmacokinetics and thus is useful as therapeutic agent for arthritis. These compounds have inhibitory effect on AP-1 activity and are useful as preventive or therapeutic agent for diseases in which excessive expression of AP-1 is involved.
    Type: Grant
    Filed: November 13, 2002
    Date of Patent: August 10, 2010
    Assignee: Toyama Chemical Co., Ltd.
    Inventors: Hisaaki Chaki, Hironori Kotsubo, Tadashi Tanaka, Yukihiko Aikawa, Shuichi Hirono, Shunichi Shiozawa
  • Publication number: 20100197502
    Abstract: The present invention relates to crystalline forms of [3-(4,5-dihydro-3-isoxazolyl)-2-methyl-4-(methylsulfonyl)phenyl]-(5-hydroxy-1-methyl-1 H-pyrazol-4-yl)methanone, which is also known under the common name topramezone. The invention also relates to a process for the preparation of these crystalline forms and formulations for plant protection which comprise one of these crystalline forms of topramezone.
    Type: Application
    Filed: July 4, 2008
    Publication date: August 5, 2010
    Applicant: BASF SE
    Inventors: Joachim Gebhardt, Peter Erk, Heidi Emilia Saxell, Thomas Kroehl, Matthias Bratz
  • Publication number: 20100179194
    Abstract: The present invention relates to novel aryl isoxazoline derivatives having excellent insecticidal activity as insecticides and represented by the formula: and their use as insecticides and acarizides.
    Type: Application
    Filed: March 28, 2008
    Publication date: July 15, 2010
    Applicant: Bayer CorpScience AG
    Inventors: Jun Mihara, Tetsuya Murata, Daiei Yamazaki, Yasushi Yoneta, Katsuhiko Shibuya, Eiichi Shimojo, Ulrich Görgens, Andreas Turberg, Thomas Bach
  • Publication number: 20100179195
    Abstract: Disclosed are compounds of Formula 1, including all geometric and stereoisomers, N-oxides, and salts thereof, wherein A is a 6-membered aromatic ring containing carbon atoms and 0-3 nitrogen atoms as ring members, said ring optionally substituted with 1-5 substituents independently selected from R2; R1 is C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C3-C6 cycloalkyl, C4-C7 alkylcycloalkyl or C4-C7 cycloalkylalkyl, each optionally substituted with one or more substituents independently selected from R21; R21 is independently H, halogen, C1-C6 alkyl, C1-C6 alkoxy, C1-C6 haloalkoxy, C1-C6 alkylthio, C1-C6 haloalkylthio, C1-C6 alkylsulfinyl, C1-C6 haloalkylsulfinyl, C1-C6 alkylsulfonyl, C1-C6 haloalkylsulfonyl, CN or NO2; and Q is as defined in the disclosure.
    Type: Application
    Filed: June 10, 2008
    Publication date: July 15, 2010
    Applicant: E.I. DUPONT DE NEMOURS AND COMPANY
    Inventors: George Philip Lahm, Ty Wagerle, Ming Xu
  • Publication number: 20100144762
    Abstract: The invention is concerned with novel sulfonamide derivatives of formula (I) wherein R2, R3, R4, A, X, Y1, Y2, Y3, Y4 and Z1 are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds inhibit L-CPT1 and can be used as medicaments.
    Type: Application
    Filed: February 8, 2010
    Publication date: June 10, 2010
    Inventors: Konrad Bleicher, Simona Maria Ceccarelli, Odile Chomienne, Patrizio Mattei, Tanja Schulz-Gasch, Christoph Martin Stahl
  • Publication number: 20100144797
    Abstract: Novel pest control agents, particularly insecticides or miticides are provided. Isoxazoline-substituted benzamide compounds of General Formula (1) or a salt thereof: (where A1, A2 and A3 are independently C or N, G is a benzene ring, etc., Q is a structure of Q-1, Q-2 or Q3: (where, for example, R1 in Q-1 is a C1 to C4 haloalkyl, etc., and R2 is H, etc., R1 in Q-2 is —OR1a, etc., R1a is a C1 to C4 alkyl, etc., and R2 is H, etc.), W is O or S, X is a halogen atom, a C1 to C2 haloalkyl, etc., Y is a halogen atom, a C1 to C2 alkyl, etc., R3 is a C1 to C2 haloalkyl, etc., m is an integer of 1-3, etc., and n is an integer of 0 or 1, etc.), and pest control agents containing the compounds.
    Type: Application
    Filed: March 6, 2008
    Publication date: June 10, 2010
    Inventors: Takeshi Mita, Yuki Furukawa, Motoyoshi Iwasa, Mitsuaki Komoda
  • Publication number: 20100144808
    Abstract: Disclosed is a novel pest control agent, in particular a pesticide or a miticide. Specifically disclosed are a substituted isoxazoline compound or a substituted enone oxime compound represented by the general formula (1) below or the general formula (2) below, and a pest control agent containing any of them. (In the formulae, the symbols are as defined in the description.
    Type: Application
    Filed: June 27, 2008
    Publication date: June 10, 2010
    Applicant: NISSAN CHEMICAL INDUSTRIES, LTD.
    Inventors: Takeshi Mita, Kenichi Toyama, Yuki Furukawa, Mitsuaki Komoda
  • Patent number: 7732472
    Abstract: The present invention relates to dihydroisoxazoles that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The invention also relates to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.
    Type: Grant
    Filed: August 15, 2005
    Date of Patent: June 8, 2010
    Assignees: Merck & Co., Inc., Merck Sharp & Dohme Corp.
    Inventors: Mark E. Fraley, Robert M. Garbaccio, George D. Hartman
  • Publication number: 20100137372
    Abstract: An isoxazoline compound represented by the formula (I): wherein the substituents are as defined in the description, has controlling activity against pests.
    Type: Application
    Filed: March 17, 2008
    Publication date: June 3, 2010
    Inventors: Hideki Ihara, Koji Kumamoto
  • Publication number: 20100137612
    Abstract: There is provided a novel intermediate for producing pesticides. A method for producing 1,3-bis(substituted phenyl)-3-substituted-3-hydroxypropan-1-one compound of Formula (3) comprises reacting an aromatic ketone compound of Formula (4) and a substituted acetophenone compound of Formula (5) as starting raw materials in an organic solvent or water in the presence or absence of an additive in the presence of a base in a suspended state. A method for producing 1,3-bis(substituted phenyl)-3-substituted-2-propen-2-one compound of Formula (2) comprises dehydrating the compound of Formula (3). A method for producing compound (2) in one step comprises reacting compound (4) and compound (5) to obtain compound (3).
    Type: Application
    Filed: June 27, 2008
    Publication date: June 3, 2010
    Applicant: Nissan Chemical Industries, Ltd.
    Inventors: Manabu Yaosaka, Tomohisa Utsunomiya, Yuji Moriyama, Tomohiro Matsumoto, Kazutaka Matoba
  • Patent number: 7728025
    Abstract: A glucokinase activator is provided; and a remedy and/or a preventive for diabetes, or a remedy and/or a preventive for diabetes such as retinopathy, nephropathy, neurosis, ischemic cardiopathy, arteriosclerosis, and further a remedy and/or a preventive for obesity are provided. A glucokinase activator characterized by containing a 2-heteroaryl-substituted benzimidazole derivative of a general formula (I-0) or its pharmaceutically-acceptable salt: [in the formula, X represents a carbon atom or a nitrogen atom; X1, X2, X3 and X4 each independently represent a carbon atom or a nitrogen atom; the ring A represents a 5- or 6-membered nitrogen-containing aromatic hetero ring of a formula (II): (in the formula, X represents a carbon atom or a nitrogen atom); R1 represents an aryl, etc.; R2 represents a hydroxy, etc.; R3 represents a —C1-6 alkyl, etc.; R4 represents a —C1-6 alkyl, etc.; X5 represents —O—, etc.
    Type: Grant
    Filed: December 28, 2004
    Date of Patent: June 1, 2010
    Assignee: Banyu Pharmaceutical Co., Ltd.
    Inventors: Katsumasa Nonoshita, Makoto Ishikawa, Hiroshi Nakashima, Daisuke Tsukahara, Yoshio Ogino, Fumiko Sakai, Yoshikazu Nagae, Keisuke Arakawa, Teruyuki Nishimura
  • Patent number: 7714142
    Abstract: To provide a method for producing a (4,5-dihydroisoxazol-3-yl)thiocarboxamidine salt compound simply, safely and in good yield, whereby drawbacks of prior art have been solved. A method for producing a (4,5-dihydroisoxazol-3-yl)thiocarboxamidine salt compound of the formula (2): wherein each of R1 and R2 which are independent of each other, is a hydrogen atom, an alkyl group or a cycloalkyl group, each of R3 and R4 which are independent of each other, is a hydrogen atom or an alkyl group, provided that R1 and R2, or R2 and R3, may be bonded to each other to form a cycloalkyl group together with the carbon atoms to which they are bonded, and X2 is a halogen or an anionic residue derived from an acid, which comprises reacting a 3-halogeno-4,5-dihydroisoxazole compound of the formula (1): wherein R1, R2, R3 and R4 are as defined above, and X1 is a halogen, with thiourea in the presence of an acid.
    Type: Grant
    Filed: December 19, 2005
    Date of Patent: May 11, 2010
    Assignee: Ihara Chemical Industry Co., Ltd.
    Inventor: Yukio Uchida
  • Publication number: 20100105920
    Abstract: A process is described for preparing isoxazoles of the formula I where the substituents are as defined below: R1 is hydrogen, C1-C6-alkyl, R2 is C1-C6-alkyl, R3, R4, R5 are hydrogen, C1-C6-alkyl, or R4 and R5 together form a bond, R6 is a heterocyclic ring, n is 0, 1 or 2; which comprises preparing an intermediate of the formula VI where R1, R3, R4 and R5 are as defined above, followed by halogenation, thiomethylation, oxidation and acylation to give compounds of the formula I. Also novel intermediates for preparing the compounds of the formula I and novel processes for preparing the intermediates are described.
    Type: Application
    Filed: January 4, 2010
    Publication date: April 29, 2010
    Inventors: Joachim Rheinheimer, Wolfgang von Deyn, Joachim Gebhardt, Michael Rack, Rene Lochtman, Norbert Götz, Michael Keil, Matthias Witschel, Helmut Hagen, Ulf Misslitz, Ernst Baumann
  • Patent number: 7696379
    Abstract: The invention provides compounds of formula (I) wherein R1 represents hydrogen or alkyl; R2 represents an unsubstituted or substituted heterocycle or R2 represents an unsubstituted or substituted aryl; R3 represents alkyl or halogen; X represents a single bond or an alkandiyl-group, optionally interrupted by one or more oxygen atoms or carbonyl groups or carbonyloxy groups in free base or acid addition salt form, processes for their preparation and their use as pharmaceuticals.
    Type: Grant
    Filed: April 24, 2006
    Date of Patent: April 13, 2010
    Assignee: Novartis AG
    Inventors: Ralf Glatthar, Thomas J. Troxler, Thomas Zoller, Joachim Nozulak
  • Patent number: 7683083
    Abstract: Biphenyl derivatives useful as ion channel antagonists are disclosed herein. The compositions thereof are useful for treating or relieving pain-related conditions.
    Type: Grant
    Filed: October 12, 2006
    Date of Patent: March 23, 2010
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Esther Martinborough, Danielle Lehsten, Timothy Neubert, Aarti Sameer Kawatkar, Nicole Zimmermann, Andreas Termin
  • Publication number: 20100048652
    Abstract: A compound of formula (I): wherein A1, A2, A3, A4, R1, R2, R3, R4, G1, G2, Q1, Y1, Y2, and Y4 are as defined in claim 1; or salts or N-oxides thereof. Furthermore, the present invention relates to processes and intermediates for preparing compounds of formula (I), to insecticidal, acaricidal, molluscicidal and nematicidal compositions comprising them and to methods of using them to combat and control insect, acarine, mollusc and nematode pests.
    Type: Application
    Filed: July 19, 2007
    Publication date: February 25, 2010
    Applicant: SYNGENTA CROP PROTECTION, INC.
    Inventors: Peter Renold, Peter Maienfisch, William Lutz, Werner Zambach
  • Patent number: 7667076
    Abstract: An amide is formed by reacting an ?-ketoacid or salt thereof in a decarboxylative condensation reaction with an amine or salt thereof comprising a nitrogen covalently bound to an atom selected from oxygen, nitrogen, and sulfur. The amide bond is formed between the ?-carbon of the ketoacid and the nitrogen of the amine. The ?-ketoacid can be formed using a novel sulfur reagent.
    Type: Grant
    Filed: September 14, 2005
    Date of Patent: February 23, 2010
    Assignee: Regents of the University of California
    Inventors: Jeffrey W. Bode, Ryan M. Fox
  • Patent number: 7662972
    Abstract: An isoxazoline-substituted benzamide compound of formula (1) or a salt thereof: wherein A1, A2 and A3 independently of one another are carbon atom or nitrogen atom, G is benzene ring, etc., X is halogen atom, C1-C6haloalkyl, etc., Y is halogen atom, C1-C6alkyl, etc., R1 is C1-C12alkyl arbitrarily substituted with R16, C3-C2alkenyl, arbitrarily substituted with R16 is oxygen atom or sulfur atom, —N(R20)R19, etc., R2 is hydrogen atom, C1-C4alkoxy C1-C6alkyl, etc., R3 is C1-C6haloalkyl, etc., R16 is halogen atom, cyano, phenyl substituted with (Z)p1, D-1 to D-60, E-1 to E-49, etc., R19 is phenyl, phenyl substituted with (Z)p1, etc., R20 is hydrogen atom, C1-C6alkyl, etc., Z is halogen atom, nitro, C1-C4alkoxy, etc., D-1 to D-60 are 5- or 6-membered aromatic heterocyclic rings, E-1 to E-49 are 5- or 6-membered saturated heterocyclic rings, m is an integer of 0 to 5, n is an integer of 0 to 4, p1 is an integer of 1 to 5. The pesticide containing these compounds.
    Type: Grant
    Filed: September 5, 2006
    Date of Patent: February 16, 2010
    Assignee: Nissan Chemical Industries, Ltd.
    Inventors: Takeshi Mita, Takamasa Kikuchi, Takashi Mizukoshi, Manabu Yaosaka, Mitsuaki Komoda
  • Patent number: 7662843
    Abstract: Methods of use and pharmaceutical compositions for a genus of low molecular weight compounds comprising optionally substituted isoxazoline ring systems that act as inhibitors of MIF (macrophage migration inhibitory factor) are disclosed. Specifically, the compounds are useful for treating a variety of diseases involving inflammatory activity or pro-inflammatory cytokine responses, such as autoimmune diseases (including rheumatiod arthritis, insulin-dependent diabetes, multiple sclerosis, graft versus host disease, lupus syndromes), asthma, arthritis, ARDS, psoriasis, interleukin-2 toxicity, proliferative vascular disease, and various forms of sepsis and septic shock, and other conditions characterized by underlying MIF responses including, for instance, tumor growth and neovascularization (angiogenesis).
    Type: Grant
    Filed: April 21, 2004
    Date of Patent: February 16, 2010
    Assignee: Cytokine PharmaSciences, Inc.
    Inventor: Yousef Al-Abed
  • Patent number: 7659294
    Abstract: The present invention encompasses compounds of Formula I: as well as the pharmaceutically acceptable salts thereof. The compounds are S1P1/Edg1 receptor agonists and thus have immunosuppressive, anti-inflammatory and hemostatic activities by modulating leukocyte trafficking, sequestering lymphocytes in secondary lymphoid tissues, and enhancing vascular integrity. The invention is also directed to pharmaceutical compositions containing such compounds and methods of treatment or prevention.
    Type: Grant
    Filed: October 18, 2005
    Date of Patent: February 9, 2010
    Assignee: Merck & Co., Inc.
    Inventors: Jeffrey John Hale, Lin Yan
  • Patent number: 7649005
    Abstract: This invention is related to compounds of general formula (I) wherein X is oxygen or sulphur or a NR7 group; R1 is C3-C8 alkyl, or C1-C8 alkyl substituted by phenoxy or phenyl, both phenoxy or phenyl being optionally substituted by one or more fluoro, chloro, trifluoromethyl, C1-C6 alkyl, hydroxyl, C1-C6 alkoxy; R2, R3 are independently hydrogen, C1-C6 alkyl, halogen, trifluoromethyl, hydroxy or C1-C6 alkoxy; R4 is hydrogen, C1-C8 alkyl; R5, R6 are independently hydrogen, C1-C3 alkyl, optionally substituted by hydroxy or phenyl; R7 is hydrogen or straight or branched C1-C3 alkyl; Het is a five to seven membered, saturated or unsaturated heteromonocyclic or an eight to ten membered, saturated or unsaturated heterobicyclic group, containing one or more heteroatoms chosen independently from nitrogen, oxygen and sulphur, said mono- or bicyclic groups being optionally substituted by C1-C6alkyl, halogen, hydroxyl or C1-C6 alkoxy; and the pharmaceutically acceptable salts or prodrug thereof, that are active as sodiu
    Type: Grant
    Filed: October 5, 2004
    Date of Patent: January 19, 2010
    Assignee: Newron Pharmaceuticals S.p.A.
    Inventors: Patricia Salvati, Carla Caccia, Piero Melloni, Alessandra Restivo, Cibele Sabido David, Stefania Vallese
  • Patent number: 7645780
    Abstract: Disclosed are compounds of the formula: where variables Z, X, R15, R2, R3, and Rc are defined herein. Compounds disclosed herein are inhibitors of the beta-secretase enzyme and are therefore useful in the treatment of Alzheimer's disease and other diseases characterized by deposition of A beta peptide in a mammal.
    Type: Grant
    Filed: June 6, 2006
    Date of Patent: January 12, 2010
    Assignee: Elan Pharmaceuticals, Inc.
    Inventors: Varghese John, Michel Maillard, James P. Beck, Eric T. Baldwin, Robert Hughes, Shon R. Pulley, Ruth T. TenBrink
  • Patent number: 7638648
    Abstract: Compounds of formulas 1 through 17 provided in the specification specifically or selectively inhibit either the cytochrome P450RAI-1 enzyme or the cytochrome P450RAI-2 enzyme.
    Type: Grant
    Filed: March 23, 2007
    Date of Patent: December 29, 2009
    Assignee: Allergan Inc.
    Inventors: Jayasree Vasudevan, Liming Wang, Xiaoxia Liu, Kwok Yin Tsang, Ling Li, Janet A. Takeuchi, Thong Vu, Richard Beard, Smita Bhat, Vidyasagar Vuligonda, Roshantha A. Chandraratna
  • Publication number: 20090318516
    Abstract: Solid forms of (1R,2S,3R)-1-(2-(isoxazol-3-yl)-1H-imidazol-4-yl)butane-1,2,3,4-tetraol and hydrates thereof are disclosed, as well as compositions comprising them and methods of their use.
    Type: Application
    Filed: June 16, 2009
    Publication date: December 24, 2009
    Inventors: Hugh Alfred Burgoon, Suzanne Marie Buttar, Christopher Stephen Frampton
  • Publication number: 20090312272
    Abstract: Transglutaminase inhibitors and methods of use thereof are provided.
    Type: Application
    Filed: August 4, 2009
    Publication date: December 17, 2009
    Inventors: Chaitan Khosla, Richard Edward Watts, Matthew John Siegel, Daniel M. Pinkas, Kihang Choi, Keith M. Rich
  • Patent number: 7629372
    Abstract: A class of compounds having Formula I and pharmaceutically acceptable salts thereof are useful as therapeutic compounds, particularly in the treatment of hyperlipidemia, hypercholesterolemia, dyslipidemia, and other lipid disorders, and in delaying the onset of or reducing the risk of developing conditions and sequelae that are associated with these diseases, such as atherosclerosis.
    Type: Grant
    Filed: September 12, 2005
    Date of Patent: December 8, 2009
    Assignee: Merck & Co., Inc.
    Inventors: James F. Dropinski, Guo Q. Shi, Yong Zhang
  • Publication number: 20090298806
    Abstract: The present invention is directed to compounds represented by Formula I and pharmaceutically acceptable salts, solvates, hydrates, and prodrugs thereof which are inhibitors of Factor Xa. The present invention is also directed to and intermediates used in making such compounds, pharmaceutical compositions containing such compounds, methods to prevent or treat a number of conditions characterized by undesired thrombosis and methods of inhibiting the coagulation of a blood sample.
    Type: Application
    Filed: January 5, 2009
    Publication date: December 3, 2009
    Inventors: Bing-Yan Zhu, Shawn M. Bauer, Zhaozhong J. Jia, Gary D. Probst, Yanchen Zhang, Robert M. Scarborough
  • Patent number: 7618973
    Abstract: The invention relates to isoxazolo-pyrazine derivatives and their pharmaceutically acceptable salts having affinity and selectivity for the GABA A ?5 receptor binding site, their manufacture, and pharmaceutical compositions containing them. The compounds of present invention are inverse agonists of GABA A ?5. The invention also relates to methods for enhancing cognition and for treating cognitive disorders like Alzheimer's disease.
    Type: Grant
    Filed: November 25, 2008
    Date of Patent: November 17, 2009
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Bernd Buettelmann, Roland Jakob-Roetne, Henner Knust, Andrew Thomas
  • Patent number: 7608564
    Abstract: Benzoyl derivatives of the formula I where the variables have the following meanings: R1, R2 are hydrogen, nitro, halogen, cyano, alkyl, haloalkyl, alkoxy, haloalkoxy, alkylthio, haloalkylthio, alkylsulfinyl, haloalkylsulfinyl, alkylsulfonyl or C1-C6-haloalkylsulfonyl; R3 is hydrogen, halogen or alkyl; R4, R5 are hydrogen, halogen, cyano, nitro, alkyl, alkoxy, alkylthio, dialkylamino, phenyl or carbonyl, it being possible for the 6 last-mentioned radicals to be substituted; X is O, S, NR9, CO or CR10R11; Y is O, S, NR12, CO or CR13R14; R15 is pyrazole which is unsubstituted or substituted, linked in the 4-position and has attached to it in the 5-position a hydroxyl or sulfonyloxy radical; and the agriculturally useful salts thereof; processes and intermediates for the preparation of the 3-heterocyclyl-substituted benzoyl derivatives; compositions comprising them; and the use of these derivatives or compositions comprising them for controlling undesirable plants.
    Type: Grant
    Filed: April 25, 2007
    Date of Patent: October 27, 2009
    Assignee: BASF Aktiengesellschaft
    Inventors: Wolfgang von Deyn, Regina Luise Hill, Uwe Kardorff, Ernst Baumann, Stefan Engel, Guido Mayer, Matthias Witschel, Michael Rack, Norbert Götz, Joachim Gebhardt, Ulf Miβlitz, Helmut Walter, Karl-Otto Westphalen, Martina Otten, Joachim Rheinheimer
  • Publication number: 20090215624
    Abstract: The invention relates to novel alkoxyalkyl spirocyclic tetramic and tetronic acids of the formula (I), in which A, B, D, Q1, Q2, Q3, Q4, G, W, X, Y and Z are as defined above, to a plurality of processes and intermediates for their preparation and to their use as pesticides and/or herbicides and/or microbicides, and also to selective herbicidal compositions comprising, firstly, the alkoxyalkyl spirocyclic tetramic and tetronic acids and, secondly, at least one crop plant compatibility-improving compound.
    Type: Application
    Filed: October 20, 2006
    Publication date: August 27, 2009
    Applicant: Bayer CropScience AG
    Inventors: Reiner Fischer, Oliver Gaertzen, Stefan Lehr, Dieter Feucht, Olga Malsam, Mark Wilhelm Drewes, Eva-Maria Franken, Christian Arnold, Thomas Auler, Martin Jeffrey Hills, Heinz Kehne, Chris Hugh Rosinger, Thomas Bretschneider, Guido Bojack, Jan Dittgen
  • Patent number: 7557133
    Abstract: The present invention relates to an isoxazoline derivative as an inhibitor against various caspases, a process for preparing the same, and a therapeutic composition for preventing inflammation and apoptosis comprising the same.
    Type: Grant
    Filed: August 26, 2004
    Date of Patent: July 7, 2009
    Assignee: LG Life Sciences Ltd.
    Inventors: Hye-Kyung Chang, Yeong-Soo Oh, Cheol-Won Park, Yong-Jin Jang, Tae-Kyo Park, Sung-Sub Kim, Min-Jung Kim, Mi-Jeong Park, Jung-Gyu Park, Hee-Dong Park, Kyeong-Sik Min, Tae-Soo Lee, Sang-Kyun Lee, Soo-Hyeon Kim, Hee-Kyung Jeong, Sun-Hwa Lee, Hwa-Dong Kim, Ae-Ri Kim, Ki-Sook Park, Hyun-Ik Shin, Hyeong-Wook Choi, Kyu-Woong Lee, Jae-Hoon Lee, Tae-Ho Heo, Ho-Jun Kim, Tae-Sik Kwon, Jeong Hui Seong
  • Patent number: 7544704
    Abstract: The present invention is concerned with aryl-4-ethynyl-isoxazole derivatives of formula I wherein R1 to R5 are as described in the specification and pharmaceutically acceptable salt thereof. This class of compounds has high affinity and selectivity for GABA A ?5 receptor binding sites, being useful as a cognitive enhancer or for the treatment of cognitive disorders like Alzheimer's disease.
    Type: Grant
    Filed: May 24, 2007
    Date of Patent: June 9, 2009
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Bernd Buettelmann, Henner Knust, Andrew Thomas
  • Publication number: 20090133319
    Abstract: Disclosed are compounds of Formula 1, including all geometric and stereoisomers, N-oxides, and salts thereof wherein A1, A2 and A3 are independently selected from the group consisting of CR3 and N; B1 B2 and B3 are independently selected from the group consisting of CR2 and N; Q is a phenyl ring or a 5- or 6-membered saturated or unsaturated heterocyclic ring, each ring optionally substituted with one or more substituents independently selected from halogen, C1-C6 alkyl, C1-C6 haloalkyl, C3-C6 cycloalkyl, C3-C6 halocycloalkyl, C1-C6 alkoxy, C1-C6 haloalkoxy, C1-C6 alkylthio, C1-C6 haloalkylthio, C1-C6 alkylsulfinyl, C1-C6 haloalkylsufinyl, C1-C6 alkylsulfonyl, C1-C6 haloalkylsulfonyl, —CN, —NO2, —N(R4)R5, —C(W)N(R4)R5, —C(O)OR5 and R8; or —S(O)2N(R21)R22; —S(O)pR25 or —S(O)(?NR28)R29; R1, R2, R3, R4, R5, R8, R21, R22, R25, R28, R29; p and n are as defined in the disclosure.
    Type: Application
    Filed: December 15, 2006
    Publication date: May 28, 2009
    Applicant: E. I. DU PONT DE NEMOURS AND COMPANY
    Inventors: George Philip Lahm, Kanu Maganbhai Patel, Thomas Francis Pahutski, JR., Benjamin Kenneth Smith
  • Publication number: 20090137647
    Abstract: Provided are various compounds of Formula I (I). Also provided are various compounds of Formula II (II). Also provided are pharmaceutical compositions comprising the above compounds. Additionally, methods of inhibiting macrophage migration inhibitory factor (MIF) activity in a mammal are provided, as are methods of treating or preventing inflammation in a mammal. Further provided are methods of treating a mammal having sepsis, septicemia, and/or endotoxic shock. Also providcd are methods of treating a mammal having an autoimmune disease, and methods of treating a mammal having a tumor.
    Type: Application
    Filed: March 23, 2007
    Publication date: May 28, 2009
    Inventor: Yousef Al-Abed
  • Patent number: 7538127
    Abstract: A compound of formula (I) or a salt, solvate, or physiologically functional derivative thereof, wherein: m is an integer of from 2 to 8; n is an integer of from 2 to 5; with the proviso that m+n is 4 to 10; R4 and R5 are independently selected from hydrogen and C1-4alkyl with the proviso that the total number of carbon atoms in R4 and R5 not more than 4; R6 and R7 are independently selected from hydrogen and C1-4alkyl with the proviso that the total number of carbon atoms in R6 and R7 is not more than 4, and Ar1 is a group selected from (a), (b), (c) and (d).
    Type: Grant
    Filed: February 12, 2004
    Date of Patent: May 26, 2009
    Assignee: Glaxo Group Limited
    Inventors: Keith Biggadike, Philip Charles Box, Diane Mary Coe, Duncan Stuart Holmes, Brian Edgar Looker, Panayiotis Alexandrou Procopiou